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TC-G-1008

Catalog No. T4648   CAS 1621175-65-2
Synonyms: GPR39-C3

TC-G-1008 (GPR39-C3) is a GPR39 (zinc receptor) agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
TC-G-1008 Chemical Structure
TC-G-1008, CAS 1621175-65-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 41.00
2 mg In stock $ 59.00
5 mg In stock $ 92.00
10 mg In stock $ 159.00
25 mg In stock $ 337.00
50 mg In stock $ 577.00
100 mg In stock $ 829.00
500 mg In stock $ 1,680.00
1 mL * 10 mM (in DMSO) In stock $ 92.00
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Purity: 99%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description TC-G-1008 (GPR39-C3) is a GPR39 (zinc receptor) agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively).
Targets&IC50 rat GPR39 :0.4 nM, human GPR39:0.8 nM
In vitro TC-G-1008 shows selectivity over a panel of kinases (IC50s>10 μM) and does not exhibit relevant binding affinity for the related ghrelin and neurotensin-1 receptors (IC50s>30 μM)[1]. GPR39-C3 is a positive allosteric modulator in HEK293-GPR39 cells which activates cAMP production (downstream of Gs), IP1 accumulation (downstream of Gq), SRF-RE-dependent transcription (downstream of G12/13), and β-arrestin recruitment. GPR39-C3 induces dose- and time-dependent loss of response in cAMP production by second challenge of the compound[2].
In vivo Rat and mouse plasma protein binding for TC-G-1008 is measured as 99.3% and 99.1%, respectively. TC-G-1008 is the first potent GPR39 agonist (EC50s ≤ 1 nM for human and rat receptor) that is orally bioavailable in mice and robustly induced acute GLP-1 levels. Upon single oral doses of 10, 30, and 100 mg/kg of aqueous suspensions in 0.5% methylcellulose/0.1% Tween 80, TC-G-1008 achieves, between 1 and 1.5 h, maximal exposures of 1.4, 6.1, and 25.3 μM, respectively[1].
Kinase Assay HEK293-GPR39 cells are plated and cultured in poly-d-lysine-coated, white, 384-well plates (4000 cells/well) in the growth medium overnight at 37°C in the presence of 5% CO2. For pretreatment of the cells with GPR39 ligands (TCG-1008) or vehicle control (DMSO), the culture medium is removed and the cells are stimulated with GPR39 ligands in assay buffer for the indicated time at 37°C. Then, the compound solution is removed and washed twice with PBS containing 0.1% BSA. For measurement of intracellular cAMP, the cells are stimulated with drugs in stimulation buffer for 30 min at 37°C. The intracellular cAMP level is determined by using HTRF cAMP dynamic 2 kit[2] .
Animal Research Mice: Mice are given single oral doses of 10, 30, and 100 mg/kg of TC-G-1008[1] .
Synonyms GPR39-C3
Molecular Weight 418.9
Formula C18H19ClN6O2S
CAS No. 1621175-65-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL

TargetMolReferences and Literature

1. Peukert S, et al. Discovery of 2-Pyridylpyrimidines as the First Orally Bioavailable GPR39 Agonists. ACS Med Chem Lett. 2014 Aug 4;5(10):1114-8. 2. Shimizu Y, et al. Rho kinase-dependent desensitization of GPR39; a unique mechanism of GPCR downregulation. Biochem Pharmacol. 2017 Sep 15;140:105-114.

Related compound libraries

This product is contained In the following compound libraries:
Orally Active Compound Library Bioactive Compound Library GPCR Compound Library NO PAINS Compound Library Bioactive Compounds Library Max

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Keywords

TC-G-1008 1621175-65-2 GPCR/G Protein GHSR inhibit GPR39-C3 TC-G 1008 Inhibitor TC-G1008 Growth hormone secretagogue receptor TC G 1008 TCG1008 inhibitor

 

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